| Identification | More | [Name]
Degrasyn (WP1130) | [CAS]
856243-80-6 | [Synonyms]
WP1130
Degrasyn
Degrasyn (WP1130)
WP1130 ( Degrasyn )
(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide Degrasyn (WP1130) | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H18BrN3O | [MDL Number]
MFCD18839228 | [MOL File]
856243-80-6.mol | [Molecular Weight]
384.27 |
| Chemical Properties | Back Directory | [density ]
1.358 | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 45 mg/ml), or in Ethanol (up to 25 mg/ml). | [form ]
solid | [color ]
Yellow | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | [InChIKey]
LIDOPKHSVQTSJY-VMEIHUARSA-N | [SMILES]
Brc1nc(ccc1)\C=C(\C(=O)N[C@@H](CCC)c2ccccc2)/C#N |
| Hazard Information | Back Directory | [Description]
WP1130 (856243-80-6) is a novel DUB inhibitor directly inhibiting USP9x, USP5, USP14 and UCH37 inducing rapid accumulation of polyubiquitinated proteins. Triggers tumor cell apoptosis.1 Blocks Jak2 signaling via Jak2 ubiquitination.2 WP-1130 causes ablation of the oncogenic transcription factor ERG in prostate cancer cells.3 See methyl analog WP1066. | [Uses]
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide can be used in biological study of drug screening and proteomic and metabolomic profiling to identify drug action mechanisms of breast cancer impaired pathogenicity. | [in vivo]
Degrasyn suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. To assess the possible therapeutic activity of Degrasyn against CML, nude mice received a subcutaneous transplant with K562 cells and are treated with 30 mg/kg Degrasyn every other day for 9 days after palpable tumor formation (10 days). This dose and schedule are well tolerated and effective in other tumor models. Antitumor activity is compared with that after daily Imatinib mesylate treatment (50 mg/kg). Nineteen days after tumor inoculation, tumors in the control group reached maximum allowable dimension, and the effect of therapy is assessed. Degrasyn treatment suppresses K562 tumor growth to an extent comparable to that observed in imatinib mesylate-treated animals, suggesting that Degrasyn is active in reducing the growth of established K562 tumors[1]. | [target]
DUB | [References]
1) Kapuria et al. (2010), Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis; Cancer Res., 70 9265
2) Kapuria et al. (2011), A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination; Cell Signal., 23 2076
3) Wang et al. (2014), Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer; Proc. Natl. Acad. Sci. USA, 111 4251 |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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